Anti-inflammatory activity of ketoprofen gel on carrageenan-induced paw edema in rats.
The anti-inflammatory activity of a 1% ketoprofen gel containing 20% Pluronic F-127 was evaluated using the carrageenan-induced rat paw edema method. The activity of the gel was compared with that of other topical nonsteroidal anti-inflammatory drug (NSAID) preparations. The Pluronic gel formulation was significantly more effective against edema formation than other ketoprofen gels used. The 1% ketoprofen gel in the Pluronic base inhibited 53% of the carrageenan-induced edema formation as compared with 38% inhibition obtained with a 3% ketoprofen gel in a Carbopol-based formulation. The topical ED50 of the 1% ketoprofen gel was 2.2 mg/kg whereas the oral ED50 of ketoprofen in a suspension was 6.1 mg/kg, indicating that the relative equiponderal availability of the topical gel was nearly three times that of the oral suspension. The application of 50 mg of the 1% ketoprofen gel on the rat hind paw at various time intervals from 0 to 24 h prior to the carrageenan injection significantly inhibited edema formation in all groups of dosed rats. A significant correlation was found between the percent inhibition of rat paw edema and the log dose of ketoprofen injected subplantarly for the dose range between 0.1 and 10 micrograms/paw.
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Department of Pharmaceutics, University of Georgia, Athens 30602.
Jun
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HW
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents; D002351:Carrageenan; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D005782:Gels; D006863:Hydrogen-Ion Concentration; D007660:Ketoprofen / Q000008:administration & dosage / Q000494:pharmacology*; D008297:Male; D011060:Poloxalene; D051381:Rats; D011919:Rats, Inbred Strains; D012869:Skin Absorption
D000893:Anti-Inflammatory Agents; D005782:Gels; D002351:Carrageenan; D011060:Poloxalene; D007660:Ketoprofen